盐酸西替利嗪咀嚼片的人体生物等效性

Study on bioequivalence of cetirizine hydrochloride chewable tablets in Chinese healthy volunteers

目的:对国产盐酸西替利嗪咀嚼片和普通片进行生物等效性考察。方法:20名健康男性志愿者按2×2交叉试验方案设计,分别口服受试制剂和参比制剂各10mg,并采集36h内动态血标本;采用高效液相色谱-质谱法测定血浆中西替利嗪浓度,计算药动学参数,并判定两种制剂是否生物等效。结果:受试制剂和参比制剂的主要药动学参数Cmax分别为(210.0±28.3)μg·L-1和(215.3±39.2)μg·L-1,tmax分别为(1.6±0.3)h和(1.60±0.20)h,AUC0-36分别为(1545.5±441.5)μg·L-1·h和(1547.4±451.1)μg·L-1·h,AUC0-∞分别为(1633.4±479.0)μg·L-1·h和(1624.0±478.6)μg·L-1·h,t1/2(ke)分别为(9.2±3.4)和(8.4±2.0)h,两制剂主要药动学参数经对数转换后进行方差分析及双单侧t检验,并计算90%置信区间,表明两种制剂生物等效,受试制剂的人体生物利用度为(100.3±12.0)%。结论:两种制剂生物等效。

OBJECTIVE To study the bioequivalence of cetirizine hydrochloride test preparation and reference preparation in Chinese healthy volunteers. METHODS 10 mg test preparation and reference preparation were given to 20 male healthy volunteers in randomized two-way crossover design for the pharmacokinetie and relative bioavailability study. Plasma concentrations of cetirizine was determined by HPLC/MS. RESULTS The main pharmacokinetics parameters of the two preparations were： Cmax （210. 0 ±28. 3）μg·L^-1 and（215.3 ±39. 2）μg·L^-1 ,tmax（1. 6 ±0. 3）h and （1.6 ±0. 2）h, AUC-36 （1 545.5 ±441.5）μg·L^-1·h and （1 547. 4 ±451.1 ）μg·L^-1·h,AUC0-∞ （1 633.4 ±479. 0）μg·L^-1·h and （ 1 624. 0 ±478. 6）μg·L^-1· h,t1/2（ke） （9. 2 -± 3.4）and （8.4±2. 0）h, respectively. The mean relative bioavailability of test preparation vs reference preparation were （100. 3 ±12. 0） %. CONCLUSION The statistical analysis shows that the two prparations are bioequivalent.